Design, synthesis and anti-influenza virus activity of furan-substituted spirothiazolidinones

Bioorg Chem. 2021 Apr 30;112:104958. doi: 10.1016/j.bioorg.2021.104958. Online ahead of print.ABSTRACTA new series of N-(3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)carboxamides have been designed, synthesized and evaluated as antiviral agents. The compounds were prepared by condensation of 2-methylfuran-3-carbohydrazide, appropriate carbonyl compounds and sulfanyl acids. The new molecules were characterized by IR, 1H NMR, 13C NMR, mass spectrometry and elemental analysis. Six analogues proved to be active against influenza A/H3N2 virus, the two most protent analogues, 3c and 3d, having an EC50 value of about 1 µM. These findings help to define the SAR of spirothiazolidinone-based inhibitors of the influenza virus membrane fusion process.PMID:33979734 | DOI:10.1016/j.bioorg.2021.104958

Source: Bioorganic Chemistry - May 12, 2021 Category: Chemistry Authors: Çağla Begüm Apaydın Merve Tansuyu Zafer Cesur Lieve Naesens F üsun Göktaş Source Type: research